32 results about "Azepindole" patented technology

This invention belongs to the field of pharmaceutical technology, specifically relating to a quinazoline-azaindole compound, its preparation method, and its application in treating Alzheimer's disease. The quinazoline-azaindole compound of this invention regulates NF-κB by inhibiting DYRK1A. k B. A series of signaling pathways, including PI3k-Akt, achieve anti-neuroinflammatory effects; quinazoline-azaindole compounds can reduce the expression of inflammatory factor-related genes in an LPS-induced BV2 microglial inflammation model, thereby reducing the levels of inflammatory factors in the hippocampus and cortex, alleviating neuronal pathological damage caused by neuroinflammation, and improving cognitive impairment caused by neuroinflammation; in summary, quinazoline compounds inhibit DYRK1A and downregulate NF-κB signaling pathways. k It can reduce the expression and release of inflammatory factors, improve brain tissue pathology, and alleviate cognitive impairment through signaling pathways such as B, and has significant clinical application value.

This invention discloses a method for synthesizing a venetum intermediate, specifically as follows: Step 1: In an organic solvent, 2,4-difluorobenzoic acid and 5-hydroxy-7-azaindole undergo an etherification reaction under the action of an acid-binding agent. After the reaction, post-treatment yields 2-((1h-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoic acid; Step 2: 2-((1h-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-fluorobenzoic acid reacts with 1-((2-(4-chlorophenyl)-4,4-dimethylcyclohexene-1-)methyl)piperazine in… An amination reaction occurs under the action of a base. After the reaction, post-treatment yields 2-(7-azaindole-5-oxy)-4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohexene-1-)methyl)piperazine-1-)benzoic acid, i.e., Venetantora intermediate III. The synthetic process provided by this invention avoids Grignard reactions and subsequent hydrolysis reactions, shortens the operation steps, simplifies the synthetic process, and provides a simple and easy-to-operate synthetic process. The raw materials are inexpensive and readily available, while avoiding the use of highly toxic raw materials. The production process is green and environmentally friendly, and suitable for industrial production.

The present invention provides compounds that inhibit rho-associated protein kinase (ROCK) for therapeutic uses as further described herein.

This invention discloses a class of indole derivatives containing or without heteroatoms (such as nitrogen heteroatoms) and their pharmaceutical compositions that can be used as PI3Kδ kinase inhibitors, and can be used to treat diseases, conditions or symptoms related to PI3Kδ inhibition, including immune disorders, cancer and cardiovascular diseases.

This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.

This disclosure relates to solid forms of (2S)-2-[(10S,17E)-16-ethoxy-6,8,10,12,20-pentamethyl-2,8,10,11,12,13-hexahydro-14H-5,3-(azenometheno)tripyrazolo[3,4-f:3',4'-j:4'',3''-n][1,4]oxazacyclopentadecin-14-yl]propan-1-ol that are useful in the treatment of disease, such as cancer, in mammals. This disclosure also relates to the preparation of such solid forms, including polymorphs, salts, cocrystals, solvates, hydrates, or a combination thereof. This disclosure also relates to compositions including such solid forms, and to methods of using such compositions in the treatment of diseases, such as cancer, in mammals, especially in humans.

Disclosed in the present invention are 7-azaindole compounds, a preparation method therefor, and the use thereof, belonging to the field of drug synthesis. The present invention particularly relates to 7-azaindole compounds containing pyrazole or indole substitution represented by general formula (I), a preparation method therefor and the use thereof in medicine. The compounds of the present invention alleviate cancer cachexia skeletal muscle atrophy by means of inhibiting ActRIIB protein in the MSTN pathway, thereby achieving a remarkable anti-cancer-cachexia effect. Experimental results show that the compounds have good anti-cachexia activity and thus can be further used for preparing novel anti-cachexia drugs.

The invention discloses a 7-azaindole compound as shown in a formula I, an optical isomer or pharmaceutically acceptable salt thereof, and also provides a preparation method and application thereof, and the obtained compound shows a certain Menin protein expression down-regulation effect, better cell proliferation inhibition activity and better PK effect.

Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

This disclosure relates to the field of anticancer drug technology, and discloses a 7-azaindole compound, its synthesis method, and its uses. The structure of the 7-azaindole compound is as follows: This 7-azaindole compound can be used as a fluorescent polarization probe or a degradation chemical probe targeting CSN5; wherein, the fluorescent polarization chemical probe has a good binding affinity to the metalloproteinase CSN5, laying an important foundation for the discovery of novel CSN5 inhibitors; at the same time, the degradation chemical probe exhibits good enzyme-level activity and cell-inhibitory activity, and has the potential to degrade CSN5 protein and its variants, providing a material basis for the development of related drugs targeting CSN5 and the study of its biological functions, and also has great potential in the discovery of cancer immunotherapy drugs and the treatment of other related diseases.

The invention relates to the technical field of biological detection and fluorescence labeling, and particularly discloses an alkynyl-substituted azaindole polymethine cyanine dye and a synthesis method and application thereof, the alkynyl-substituted azaindole polymethine cyanine dye has a structure as shown in the following general formula I: in the general formula I, X is selected from H, F, Cl, Br or I; y is a C or N atom; n is an integer of 0, 1 or 2; r1, R3, R5 and R6 are respectively and independently selected from hydrogen, C-Calkyl, C-Ccarboxy alkyl, aryl, aryl carboxylic ester, C-Calkyl sulfonate, aryl sulfonate, C-Calkyl sulfonamide or aryl sulfonamide; r2 and R4 are respectively and independently selected from hydrogen, halogen,-COOH,-NHH,-SOH,-SONHH, C-Calkyl carboxylic ester, C-Camino alkyl, aryl, aryl carboxylic ester, C-Calkyl sulfonate, aryl sulfonate, C-Calkyl sulfonamide or aryl sulfonamide.

The application discloses a kind of chiral 7-azaindoline amide compounds, its synthesis method and application, belong to organic chemistry synthesis and medical technology field, the compound has with N-[3-phenyl-3-(diphenyl phosphoryl) propionyl] Substituted 7-azaindoline as basic skeleton Structural characteristics;Its synthesis method is: under room temperature condition, copper salt is dissolved in organic solvent with chiral ligand (L) Stirring mixing, then sequentially adding α, β-unsaturated 7-azaindoline amide (I), diphenyl phosphine (II) And base, after stirring reaction, the target product is obtained by separation and purification;The compound provided by the application can be efficiently converted into other novel 7-azaindoline derivatives by simple reaction, and has potential application value in the field of medicinal chemistry and asymmetric catalysis;The synthesis method provided by the application has the advantages of simple operation, mild reaction condition, wide substrate applicability, high yield and high enantioselectivity.

The application discloses a 7-azaindole photoacoustic imaging probe for detecting superoxide anion, a preparation method and application, and the photoacoustic imaging probe is named AIH-OTF, which is a blue-green solid prepared from methyl trifluoromethanesulfonate, dye AIH-OH and the like; the AIH-OTF realizes high-contrast PA imaging of endogenous superoxide anion in living cells, and in-situ evaluation of occurrence and repair of acetaminophen-induced liver injury is also determined through non-invasive monitoring of the PA reaction of AIH-OTF to superoxide anion; the AIH-OTF probe can be used as a useful tool for accurately diagnosing drug-induced liver injury in vivo. The photoacoustic imaging probe can realize real-time detection of in-vivo superoxide anion through AIH-OTF and the ability of diagnosing DILI; the cell toxicity is small, the biological compatibility is good, and the photoacoustic imaging probe can be used for in-vivo imaging of occurrence and repair of DILI.

This invention relates to the fields of organic light-emitting materials and tumor drugs, and particularly to a benzozaindolone compound, its preparation method, and its application. The structural formula of the benzozaindolone compound is shown in formula (3). This invention adopts a one-step synthesis strategy, which is simple, mild, has inexpensive and widely available substrates, and has a high conversion yield. It provides a simple and green synthetic approach for the synthesis of benzozaindolone compounds. Furthermore, the target compound (benzozaindolone compound) has excellent fluorescence luminescence properties and biocompatibility, and can be directly applied to fluorescence imaging of cancer cells and type I photodynamic therapy.

The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).

The invention discloses a green and efficient synthesis method of high-purity 4-chloro-5-fluoro-7-azaindole, which comprises the following steps: by taking 5-fluoro-1H-pyrrolo [2, 3-B] pyridine as a raw material, carrying out high-selectivity reaction on the 5-fluoro-1H-pyrrolo [2, 3-B] pyridine and a composite chlorination system consisting of phosphorus oxychloride and N, N-dimethylformamide in an aprotic polar solvent under the catalysis of Lewis acid, thereby obtaining the high-purity 4-chloro-5-fluoro-7-azaindole. After the reaction is completed, an integrated quenching-neutralization-extraction post-treatment process is adopted, the operation is simplified, and a crude product is finally recrystallized and purified through a stepped solvent system consisting of ethyl acetate, methyl tert-butyl ether and normal hexane. According to the method, chlorination sites are accurately controlled by optimizing a reaction system, so that by-products are remarkably reduced; meanwhile, the used raw materials and solvents are economical and environment-friendly, and the catalyst is high in efficiency and suitable for industrial production.

Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

This invention provides methods of treating selected rho-associated protein kinase (ROCK) mediated disorders comprising administering an effective amount of a compound of Formula I, Formula II, or Formula III to a human patient in need thereof as described further herein.

The present invention concerns a compound of formula (I):or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity, in particular ERK2 activity.

This invention relates to 7-azaindole compounds I-1–I-5, their preparation methods, and their applications in the prevention and control of plant viral and fungal diseases. This invention provides a series of 7-azaindole compounds, develops efficient synthetic methods for these compounds, and discovers their antiviral and antipathogenic activities, laying the foundation for the synthesis and bioactivity research of these compounds. The 7-azaindole compounds I-1–I-5 of this invention exhibit antiviral activity, inhibiting tobacco mosaic virus, and also demonstrate broad-spectrum antipathogenic activity.

The present application relates to a kind of 7-azaindole derivatives and its use. Particularly, the present application relates to the compound shown in general formula (I), its preparation method, its pharmaceutical composition, and the use of the compound shown in general formula (I) or its pharmaceutical composition, the compound can be used as the drug for preventing and / or treating ActR II mediated related diseases, wherein each substituent in general formula (I) is the same as defined in the specification.

The invention belongs to the technical field of medicines, and particularly relates to a 4-substituted-2-biphenyl-7-azaindole compound and application of the 4-substituted-2-biphenyl-7-azaindole compound as a CSN5 inhibitor. The invention provides a series of 4-substituted-2-biphenyl-7-azaindole compounds as shown in a formula I. The compounds have good CSN5 inhibitory activity and are expected to be used as drugs for preventing and treating CSN5-mediated diseases (such as cancers). The invention provides a new choice for clinical medication, and has a good application prospect.

This application discloses a compound that has inhibitory activity against LRRK2. This application also discloses a pharmaceutical composition comprising the compound and a method of treating diseases and conditions using the compound, said diseases and conditions including neurodegenerative diseases and conditions such as Parkinson's disease and brain cancers (e.g., glioma and glioblastoma).

The disclosure provides Group 6 complexes, which, in some embodiments, are useful for catalyzing olefin metathesis reactions. In some embodiments, the compounds are compounds of the following formula: wherein: M is a Group 6 metal atom; X is an oxygen atom, =N-R5, =N-N(R5)(R5') or =N-0-R5, R5 and R5' independently being various substituents, such as aryl or heteroaryl, each optionally substituted; n is 0 or 1; Rz is a neutral ligand; R1 is hydrogen or an organic substituent; R2 is an aryl or heteroaryl group, each optionally substituted; R3 is an anionic ligand; and R4 is an anionic ligand, such as a pyrrolide, a pyrazolide, an imidazolide, an indolide, an azaindolide, or an indazolide, each optionally substituted.

The application discloses a substituted 7-azaindole-3-carboxylic acid Mcl-1 protein inhibitor and a preparation method and application thereof, and the compound has a structure as shown in a general formula I. The compound has strong inhibitory activity on Mcl-1 protein, can prevent or treat related mammal diseases caused by abnormal expression of Mcl-1 protein, and the application also relates to a pharmaceutical use of a composition with the compound of the general formula I.

The application discloses a preparation method of N-(2-acetylamino phenyl)-7-azaindole. The method can efficiently and in high yield prepare N-(2-acetylamino phenyl)-7-azaindole through one-step reaction under mild conditions, by taking N-phenyl-7-azaindole and 3-methyl-1,4,2-dioxazol-5-ketone as raw materials, [Ru(p-cymene)Cl2]2 as a main catalyst, AgNTf2 as a cocatalyst, and an alkali metal acetate as a reaction aid.

The present invention relates to a compound represented by general formula (1) or a pharmaceutically acceptable salt thereof. [In general formula (1), R1 represents a group represented by general formula (2) or general formula (3), R2 represents a hydrogen atom or the like, R3 represents a substituted or unsubstituted aryl group or the like, R4 represents a halogen, R5 represents a substituted or unsubstituted aryl group or the like, R6 and R7 each independently represent a hydrogen atom or the like, R8 represents a substituted or unsubstituted aryl group or the like, R9 and R10 each independently represent a substituted or unsubstituted alkyl group or the like, and R7 represents a halogen atom or the like. R9 and R10 may be linked to each other to form a ring, and R11 represents a substituted or unsubstituted aryl group or the like. ] [chemical 1] [chemical 2] [chemical 3]

This invention provides azaindole rho-associated protein kinase (ROCK) inhibiting compounds for treating disorders mediated by ROCK1 and / or ROCK2, such as a neurodegenerative disease or disorder, a kidney disease, a cancer, or a fibrotic disease or disorder, in a subject in need thereof. Specifically disclosed are compounds with a pyrrolo[2,3- b]pyridine-2-carboxamide structural backbone comprising a substituted pyrazolyl moiety at the 6-position.